Tag: 200-300

On September 2, 2015, Cheng, Guolin; Li, Tuan-Jie; Yu, Jin-Quan published an article.Electric Literature of 5455-98-1 The title of the article was Practical Pd(II)-Catalyzed C-H Alkylation with Epoxides: One-Step Syntheses of 3,4-Dihydroisocoumarins. And the article contained the following:

Pd(II)-catalyzed ortho-alkylation of benzoic acids with both terminal and internal epoxides affords 3,4-dihydroisocoumarins I [ R1 = Me, F, Cl, etc; R = H, Me, Bn, etc] in one step. The presence of potassium countercations is crucial for this reaction. Monoprotected amino acid ligands significantly promote this reaction, enabling the development of a practical C-H alkylation reaction using 0.5 mol % Pd catalyst. The inversion of stereochem. in the C-H alkylation step is consistent with a redox-neutral SN2 nucleophilic ring-opening process as opposed to a Pd(II)/Pd(IV) pathway. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Electric Literature of 5455-98-1

The Article related to benzoic acid epoxide alkylation palladium catalyst, dihydroisocoumarin preparation, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Electric Literature of 5455-98-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 31, 2019, Vadivelu, Saravanan; Rajagopal, Sridharan; Burri, Raghunadha Reddy; Garapaty, Shivani; Sivanandhan, Dhanalakshmi; Thakur, Manish Kumar; Natarajan, Tamizharasan; Swamy, Indu N.; Nagaraju, Nagendra; Kanagaraj, Subramaniam; Mohd, Zainuddin; Sarkar, Sayantani; Samanta, Swapan Kumar; Hariprakash published a patent.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the patent was Preparation of heterocyclic compounds as PRMT5 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof as PRMT5 inhibitors; their preparation and use in the treatment of and/or prevention of various diseases, including cancer and infectious diseases. Compounds of formula I wherein A is substituted isoquinolinyl, dihydroindenylamino; dashed bond is optional single or double bond; n = 0-1; m = 0-2; p = 1-2; q = 1-3; R1 – R6 are independently H, halo, OH, etc.; R7 is H, C1-6 (un)substituted alkyl, (un)substituted aryl, etc.; R8 is absent, H, halo, C1-6 alkyl, etc.; R10 is H, halo, OH, CN, etc.; X, Y and Z are independently NH and derivatives, O, S, etc.; W and B are independently N and C; and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof, are claimed. Example compound II was prepared by amidation of 6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-carboxylic acid with 1-amino-3-(3,4-dihydroisoquinolin-2(1H)-yl)propan-2-ol. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value ranged from 0.01-1 μM. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to heterocycle preparation prmt5 inhibitor treatment cancer infection, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 31, 2019, Vadivelu, Saravanan; Rajagopal, Sridharan; Burri, Raghunadha Reddy; Garapaty, Shivani; Sivanandhan, Dhanalakshmi; Thakur, Manish Kumar; Natarajan, Tamizharasan; Swamy, Indu N.; Nagaraju, Nagendra; Kanagaraj, Subramaniam; Mohd, Zainuddin; Sarkar, Sayantani; Samanta, Swapan Kumar; Hariprakash published a patent.COA of Formula: C11H9NO3 The title of the patent was Preparation of heterocyclic compounds as PRMT5 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof as PRMT5 inhibitors; their preparation and use in the treatment of and/or prevention of various diseases, including cancer and infectious diseases. Compounds of formula I wherein A is substituted isoquinolinyl, dihydroindenylamino; dashed bond is optional single or double bond; n = 0-1; m = 0-2; p = 1-2; q = 1-3; R1 – R6 are independently H, halo, OH, etc.; R7 is H, C1-6 (un)substituted alkyl, (un)substituted aryl, etc.; R8 is absent, H, halo, C1-6 alkyl, etc.; R10 is H, halo, OH, CN, etc.; X, Y and Z are independently NH and derivatives, O, S, etc.; W and B are independently N and C; and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof, are claimed. Example compound II was prepared by amidation of 6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-carboxylic acid with 1-amino-3-(3,4-dihydroisoquinolin-2(1H)-yl)propan-2-ol. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value ranged from 0.01-1 μM. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).COA of Formula: C11H9NO3

The Article related to heterocycle preparation prmt5 inhibitor treatment cancer infection, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.COA of Formula: C11H9NO3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On December 14, 2017, Ombrato, Rosella; Magaro’, Gabriele; Garofalo, Barbara; Furlotti, Guido; Mangano, Giorgina; Capezzone de Joannon, Alessandra published a patent.Category: amides-buliding-blocks The title of the patent was Preparation of fused hetereocyclic compounds as antibacterial agents. And the patent contained the following:

The invention relates to novel antibacterial compounds of formula A-L1-Y-L2-R-B (wherein A is cyclic group; L1 is σ bond, (un)substituted C1-3 alkylenyl; Y is piperidinyl, piperazinyl, pyrrolidinyl, etc.; L2 is σ bond, (un)substituted C1-3 alkylenyl, NH and derivatives, etc.; R is α bond and heterocyclyl; B is substituted benzopyranopyrrolyl), and addition salts with pharmaceutically acceptable organic or inorganic acids or basis, enantiomers, N-oxides and quaternary ammonium salts thereof, pharmaceutical compositions containing them and their use as antimicrobials. Example compound I was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their antibacterial activities (data given). The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Category: amides-buliding-blocks

The Article related to fused hetereocyclic compound antibacterial agent preparation, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On December 14, 2017, Ombrato, Rosella; Magaro, Gabriele; Garofalo, Barbara; Furlotti, Guido; Mangano, Giorgina; Capezzone de Joannon, Alessandra published a patent.Name: 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the patent was Preparation of fused heterocyclic compounds as antibacterial agents. And the patent contained the following:

The invention relates to novel antibacterial compounds of formula A-L1-Y-L2-R-B (wherein A is cyclic group; L1 is σ bond, (un)substituted C1-3 alkylenyl; Y is piperidinyl, piperazinyl, pyrrolidinyl, etc.; L2 is σ bond, (un)substituted C1-3 alkylenyl, NH and derivatives, etc.; R is α bond and heterocyclyl; B is substituted benzopyranopyrrolyl), and addition salts with pharmaceutically acceptable organic or inorganic acids or basis, enantiomers, N-oxides and quaternary ammonium salts thereof, pharmaceutical compositions containing them and their use as antimicrobials. Example compound I was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their antibacterial activities (data given). The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Name: 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to fused heterocyclic compound antibacterial agent preparation, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Name: 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 29, 2020, Zhang, Guofu; Cui, Yin; Zhao, Yiyong; Cui, Yunqiang; Bao, Shenxiao; Ding, Chengrong published an article.Category: amides-buliding-blocks The title of the article was A Practical Approach to Ureas and Thiocarbamates: SO2F2-Promoted Lossen Rearrangement of Hydroxamic Acid. And the article contained the following:

A simple, mild and practical method for the synthesis of sym. urea ArNHC(O)NHAr (Ar = C6H5, 1-naphthyl, 2-pyridyl, etc.) via Lossen rearrangement promoted by SO2F2, which achieves the conversion from hydroxamic acid ArC(O)NHOH to sym. urea in high selectivity and provides a new method for facile initiation of Lossen rearrangement has been described. Meanwhile, the reaction within amines R1NHR2 (R1 = 4-CH3OC6H4, 4-ClC6H4, C6H5CH2; R2 = H, Me) or thiols like 4-methylbenzene-1-thiol and phenylmethanethiol also provide the efficient synthetic strategy towards unsym. ureas C6H5NHC(O)NR1R2 or thiocarbamates like S-(p-tolyl) phenylcarbamothioate and S-benzyl phenylcarbamothioate. Significant for gram-scale application, the desired product on gram-scale by filtration without further purifn was afforded. A plausible mechanism which is supported by control exptl. and spectral data is proposed. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Category: amides-buliding-blocks

The Article related to urea preparation, hydroxamic acid lossen rearrangement, amine hydroxamic acid lossen rearrangement, thiocarbamate preparation, thiol hydroxamic acid lossen rearrangement, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Song, Xizhong; Liu, Xiaoyu; Yu, Wei; Jin, Yi published an article in 2021, the title of the article was Amide-Assisted Rearrangement of Hydroxyarylformimidoyl Chloride to Diarylurea.HPLC of Formula: 102-07-8 And the article contains the following content:

A novel amide-assisted rearrangement reaction of hydroxybenzimidoyl chloride was established for the efficient synthesis of 1,3-diphenylurea derivatives A variety of electronically and sterically different 1,3-diphenylurea derivatives could be obtained in good to excellent yields, and a proposed reaction mechanism was also presented. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).HPLC of Formula: 102-07-8

The Article related to hydroxyarylformimidoyl chloride rearrangement, diphenylurea preparation, diarylurea, benzamide, hydroxyarylformimidoyl chloride, rearrangement, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.HPLC of Formula: 102-07-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On August 26, 2022, Joseph, Devaneyan; Lee, Sunwoo published an article.Application In Synthesis of 1,3-Diphenylurea The title of the article was Reaction of Amide and Sodium Azide for the Synthesis of Acyl Azide, Urea, and Iminophosphorane. And the article contained the following:

Amides reacted with NaN3 to give the acyl azides in DMF at 25°C and produce the sym. ureas in THF/H2O at 80°C via the sequential reaction of acyl substitution and Curtius rearrangement. All acyl azides were also obtained from the secondary amides via sequential reaction of p-toluenesulfonyl chloride and NaN3. In addition, keto-stabilized iminophosphoranes were prepared from a one-pot reaction of amides, NaN3, and phosphines. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Application In Synthesis of 1,3-Diphenylurea

The Article related to acyl azide sym aromatic urea iminophosphorane preparation, amide sodium azide phosphine substitution curtius rearrangement, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.Application In Synthesis of 1,3-Diphenylurea

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 31, 2021, Harish, N.; Kathyayini, N.; Baby, Bindhu; Nagaraju, N. published an article.Application of 102-07-8 The title of the article was Investigation of active sites using solid state 27Al and 31P MAS NMR in ceramic amorphous aluminophosphate materials prepared from different potassium salts of phosphate for the synthesis of diphenyl urea derivatives. And the article contained the following:

Ceramic amorphous aluminophosphate (CAmAlP) catalysts were prepared by precipitation method using different phosphate salts of potassium such as KH2PO4, K4P2O7 and K2HPO4 as well as H3PO4. The prepared materials were characterized by PXRD, FT-IR, XPS, SEM, BET Surface area, NH3-TPD, 27Al NMR and 31P NMR anal. methods. The catalytic activity of the materials was checked in the synthesis of di-Ph urea (DPU) from aniline and di-Et carbonate, under refluxing conditions. Further, the general application of the catalysts was tested using various substituted anilines. The recyclability of the catalysts was also studied. Uncertainties in percentage yields were calculated to check the reproducible surface properties. The P-XRD, BET Surface area and NH3-TPD results indicated that the materials were amorphous with mesoporous texture, surface areas and acidities in the range 200-260 m2/g and 0.4-0.7 mmol/g resp. 27Al NMR studies revealed that Al was present in three different coordination states such as tetrahedral, pentagonal and octahedral. The relative percentages of these Al sites depended on the type of the potassium precursor phosphate salt used. Both tetrahedral and pentagonal Al sites in conjunction with each other represented catalytically active sites. An increase in the pentagonal sites contributed to addnl. increments to the catalytic activity of CAmAlP. The catalyst prepared from KH2PO4 was found to be the best and demonstrated 96% DPU yield. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Application of 102-07-8

The Article related to diphenyl urea preparation, aniline diethyl carbonate condensation ceramic amorphous aluminophosphate catalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ureas, Carbamic Acids, Guanidines, and Their Sulfur-Containing Analogs and other aspects.Application of 102-07-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kakeya, Nobuharu; Yata, Noboru; Kamada, Akira; Aoki, Masaru published an article in 1969, the title of the article was Biological activities of drugs. VII. Structure-activity relations of sulfonamide carbonic anhydrase inhibitors. 2.Application of 97-09-6 And the article contains the following content:

Diuretic, natriuretic activities, and duration of the diuretic action in rats were studied with 22 sulfonamide derivatives To clarify the active form of the sulfonamides, the effect of pH of the rat body fluid on the diuretic activity was studied. The diuretic and natriuretic activities of the sulfonamides increased with an increase in their carbonic anhydrase inhibitory activity except for o-substituted benzenesulfonamides, disubstituted benzenesulfonamides, and 2-amino-1,3,4-thiadiazole-5-sulfonamide. A close relation between diuretic and natriuretic activities with the electronic characteristics of the sulfamoyl group, such as Hammett’s σ constant, pKa, NMR chem. shift of the sulfamoyl protons, and S:O valence-force constant was observed for the derivatives with some exceptions. A compound having a large partition coefficient and strong albumin binding ability showed long duration of the diuretic action. The diuretic and natriuretic activities of sulfonamides were enhanced by an increase in their dissociation constants The diuretic activity was enhanced under alkaline conditions. It was concluded that the active form of the sulfonamide carbonic anhydrase inhibitors was the ionized form. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application of 97-09-6

The Article related to sulfonamides diuresis natriuresis, diuresis natriuresis sulfonamides, natriuresis sulfonamides diuresis, carbonic amhydrase drug, amhydrase carbonic drug, drug carbonic anhydrase and other aspects.Application of 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics